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macitentan
EntityQ6724151· pop 12· linked from 159 articles

macitentan

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Also known as ACT-064992, ACT064992, ACT 064992

Macitentan, sold under the brand name Opsumit, is an endothelin receptor antagonist developed by Actelion and approved for the treatment of pulmonary arterial hypertension (PAH). Macitentan is a dual endothelin receptor antagonist, meaning that it acts as an antagonist of two endothelin (ET) receptor subtypes, ETA and ETB. However, macitentan has a 50-fold increased selectivity for the ETA subtype compared to the ETB subtype.

Wikidata facts

Mass
585.9633483200003
Has use
medication
Show 7 more facts
chemical formula
C₁₉H₂₀Br₂N₆O₄S
canonical SMILES
CCCNS(=O)(=O)NC1=C(C(=NC=N1)OCCOC2=NC=C(C=N2)Br)C3=CC=C(C=C3)Br
World Health Organisation international non-proprietary name
macitentan
defined daily dose
10
medical condition treated
pulmonary hypertension
Commons category
Macitentan
legal status (medicine)
boxed warning
Sources (7)

via Wikidata · CC0

~4 min read

Encyclopedic overview

7 sections
Contents
  • Adverse effects
  • Mechanism of action
  • Endothelin and endothelin receptors
  • Role of macitentan
  • Pharmacokinetics
  • Experimental pharmacokinetics
  • References

Macitentan, sold under the brand name Opsumit, is an endothelin receptor antagonist developed by Actelion and approved for the treatment of pulmonary arterial hypertension (PAH). Macitentan is a dual endothelin receptor antagonist, meaning that it acts as an antagonist of two endothelin (ET) receptor subtypes, ETA and ETB. However, macitentan has a 50-fold increased selectivity for the ETA subtype compared to the ETB subtype.

Macitentan was approved for medical use in the United States in October 2013.

Excerpted from Wikipedia’s “macitentan” article, available under the CC BY-SA 4.0 licence.